Trimebutine has been used for treatment of both hypermotility and hypomotility disorders of the gastrointestinal (GI) tract, such as irritable bowel syndrome. In this issue, Tan et al. (2011) examined the concentration-dependent dual effects of trimebutine on colonic motility in guinea pig. The authors suggested that trimebutine attenuated colonic motility mainly through the inhibition of L-type Ca(2+) channels at higher concentrations, whereas, at lower concentrations, it depolarized membrane potentials by reducing BK(ca) currents, resulting in the enhancement of the muscle contractions. Trimebutine might be a plausible modulator of GI motility, which gives an insight in developing new prokinetic agents. Further studies to elucidate the effects of trimebutine on the interstitial cells of Cajal, the pacemaker in GI muscles would promote the therapeutic benefits as a GI modulator.